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1.
Assay Drug Dev Technol ; 18(4): 195-201, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32392426

RESUMO

Due to the increasing resistance of various Candida species to azole drugs, particularly fluconazole, it would be of significant importance to look for alternative therapies. The aim of this study was to investigate the antifungal activity of capric acid and its in vitro interactions with nystatin and fluconazole against Candida isolates. A total of 40 Candida isolates (C. albicans, 36; C. kefyr, 2; C. tropicalis, 1; C. glabrata, 1) collected from the oral cavity of neonates with oropharyngeal candidiasis and a reference strain of C. albicans (ATCC 10231) were used in this study. Antifungal activity of capric acid and two comparator antifungal drugs, namely fluconazole and nystatin, was tested according to CLSI M27-A3/M60 method. The in vitro interaction between capric acid with fluconazole and nystatin was determined following a checkerboard method and results were interpreted using fractional inhibitory concentration index. Nystatin had the lowest minimum inhibitory concentrations (range, 0.125-8 µg/mL; geometric mean [GM], 0.6229 µg/mL) followed by fluconazole (range, 0.5-16 µg/mL; GM, 1.9011 µg/mL) and capric acid (range, 128-2,048 µg/mL; GM, 835.9756 µg/mL). When tested in combination, capric acid with fluconazole demonstrated synergistic, indifferent, and antagonistic interactions in 3 (7.317%), 24 (58.536%), and 14 (34.146%) cases, respectively. For combination of capric acid with nystatin, synergistic, indifferent, and antagonistic interactions were observed in 1 (2.439%), 19 (46.341%), and 21 (51.219%) cases, respectively. All cases of synergistic interactions were against resistant or susceptible dose-dependent isolates. Fluconazole, nystatin, and capric acid seem to be more effective when they are used alone compared with their combination. However, their combination might be effective on resistant isolates.


Assuntos
Antifúngicos/farmacologia , Candida/efeitos dos fármacos , Candidíase Bucal/tratamento farmacológico , Ácidos Decanoicos/farmacologia , Fluconazol/farmacologia , Nistatina/farmacologia , Antifúngicos/química , Antifúngicos/isolamento & purificação , Candida/isolamento & purificação , Candidíase Bucal/microbiologia , Ácidos Decanoicos/química , Ácidos Decanoicos/isolamento & purificação , Relação Dose-Resposta a Droga , Fluconazol/química , Fluconazol/isolamento & purificação , Humanos , Testes de Sensibilidade Microbiana , Nistatina/química , Nistatina/isolamento & purificação
2.
J Pharm Pharmacol ; 69(11): 1578-1591, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28809438

RESUMO

OBJECTIVES: This study was carried out to investigate the impact of various isolated phytochemical components present in the Wattakaka volubilis leaves for the growth and proliferation of human osteoblast like cells (MG63). KEY FINDINGS: Ethyl acetate was found to be the best solvent for potential extraction of phytocompounds. Further, the MTT assay was carried out to deduce the viability of 44 isolated phytochemicals. Ten phytochemical fractions found to increase the cell growth were subjected to statistical tool namely Plackett-Burman and Central composite design to screen the optimum phytochemical fraction and its dosage. The active phytochemical constituents were analysed and identified as hexadeconoic acid, octadeconoic acid, N,N-diisopropyl(2,2,3,3,3-pentafluoropropyl)amine using GC-MS and HPLC techniques. The impact of optimized concentration was assessed on osteoblast cells. The maximum % cell viability, % DNA and collagen content were found to be 164.44, 159.32 and 3.81, respectively. CONCLUSIONS: The results confirmed that the optimized fraction containing decanoic acid and isopropyl amine at particular concentration stimulated the proliferation of human osteoblast (MG63) cells. Hence, the optimized concentration of this compound from W. volubilis may used for treatment of bone related injuries externally.


Assuntos
Apocynaceae/química , Proliferação de Células/efeitos dos fármacos , Osteoblastos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Cromatografia Líquida de Alta Pressão , Colágeno/metabolismo , Ácidos Decanoicos/química , Ácidos Decanoicos/isolamento & purificação , Ácidos Decanoicos/farmacologia , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Osteoblastos/metabolismo , Extratos Vegetais/química , Folhas de Planta , Propilaminas/química , Propilaminas/isolamento & purificação , Propilaminas/farmacologia
3.
Nat Prod Commun ; 4(3): 389-94, 2009 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-19413119

RESUMO

Two antifouling compounds, aureobasidin (1), a new ester with an unusual 4,6-dihydroxydecanoic acid residue, and (3R,5S)-3,5-dihydroxydecanoic acid (2), were isolated from the marine-derived fungus Aureobasidium sp., in addition to (5R,3Z)-5-hydroxydec-3-enoic acid (3) and (R)-3-hydroxydecanoic acid (4). The structures were unambiguously established by IR, 1D and 2D NMR spectroscopic and mass spectral data. Compounds 1-3 were found to be active against Bacillus subtilis, Escherichia coli and Staphyllococcus aureus. Compound 3 showed fungistatic activity against Candida albicans.


Assuntos
Ascomicetos/química , Ácidos Decanoicos/análise , Ácidos Decanoicos/isolamento & purificação , Ésteres/análise , Ésteres/isolamento & purificação , Bacillus subtilis/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Ácidos Decanoicos/farmacologia , Escherichia coli/efeitos dos fármacos , Ésteres/farmacologia , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Staphylococcus aureus/efeitos dos fármacos
4.
J Antibiot (Tokyo) ; 53(8): 788-92, 2000 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-11079800

RESUMO

A new metabolite, diheteropeptin, was found in the culture broth of Diheterospora chlamydosporia Q58044 by screening for TGF-beta-like active substances. Diheteropeptin was extracted from the culture supernatant and purified by a series of chromatographies such as silica gel, gel filtration and HPLC. Diheteropeptin exhibited cytostatic activity in Mv1Lu cells with an IC50 value of 20.3 microM and inhibited histone deacetylase.


Assuntos
Ácidos Decanoicos/isolamento & purificação , Ácidos Decanoicos/farmacologia , Hypocreales/metabolismo , Peptídeos , Antibacterianos/farmacologia , Divisão Celular/efeitos dos fármacos , Células Cultivadas , Ácidos Decanoicos/metabolismo , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos/métodos , Inibidores Enzimáticos/farmacologia , Fermentação , Inibidores de Histona Desacetilases , Humanos , Concentração Inibidora 50 , Fator de Crescimento Transformador beta/farmacologia
5.
Chem Pharm Bull (Tokyo) ; 45(12): 1955-60, 1997 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-9433765

RESUMO

Alkaline hydrolysis of the ether-soluble resin glycoside fraction of seeds of Quamoclit (Q.) x multifida, a hybrid between Q. pinnata and Q. coccinea, gave new glycosidic acids, multifidinic acids A and B, along with two known glycosidic acids, quamoclinic acid A and operculinic acid A, and three organic acids, (2S)-2-methylbutyric acid, n-decanoic acid and n-dodecanoic acid. Further, as major ether-soluble resin glycosides, new jalapins named multifidins I and II, were isolated accompanied by quamoclins I-IV, which were previously obtained from seeds of Q. pinnata. The structures of multifidins I and II, and multifidinic acids A and B have been determined on the basis of chemical and spectral data.


Assuntos
Glicosídeos/isolamento & purificação , Lactonas/isolamento & purificação , Oligossacarídeos/isolamento & purificação , Plantas/química , Butiratos/química , Ácido Butírico , Sequência de Carboidratos , Ácidos Decanoicos/isolamento & purificação , Lactonas/química , Ácidos Láuricos/isolamento & purificação , Espectroscopia de Ressonância Magnética , Dados de Sequência Molecular , Oligossacarídeos/química , Extratos Vegetais/química , Resinas Vegetais , Ramnose/química , Sementes/química
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